SG177646A1 - Gpr119 agonists - Google Patents
Gpr119 agonists Download PDFInfo
- Publication number
- SG177646A1 SG177646A1 SG2012002523A SG2012002523A SG177646A1 SG 177646 A1 SG177646 A1 SG 177646A1 SG 2012002523 A SG2012002523 A SG 2012002523A SG 2012002523 A SG2012002523 A SG 2012002523A SG 177646 A1 SG177646 A1 SG 177646A1
- Authority
- SG
- Singapore
- Prior art keywords
- mmol
- methanesulfonyl
- tetrahydro
- mixture
- added
- Prior art date
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- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 1
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- 230000003914 insulin secretion Effects 0.000 description 1
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- 238000004811 liquid chromatography Methods 0.000 description 1
- 238000001294 liquid chromatography-tandem mass spectrometry Methods 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 239000012139 lysis buffer Substances 0.000 description 1
- NXPHGHWWQRMDIA-UHFFFAOYSA-M magnesium;carbanide;bromide Chemical compound [CH3-].[Mg+2].[Br-] NXPHGHWWQRMDIA-UHFFFAOYSA-M 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- PAWUSHZXEZPDBE-UHFFFAOYSA-N methyl 1-(trifluoromethyl)cyclopropane-1-carboxylate Chemical compound COC(=O)C1(C(F)(F)F)CC1 PAWUSHZXEZPDBE-UHFFFAOYSA-N 0.000 description 1
- RZVWBASHHLFBJF-UHFFFAOYSA-N methyl piperidine-4-carboxylate Chemical compound COC(=O)C1CCNCC1 RZVWBASHHLFBJF-UHFFFAOYSA-N 0.000 description 1
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- 150000004712 monophosphates Chemical class 0.000 description 1
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- 235000019799 monosodium phosphate Nutrition 0.000 description 1
- 239000012452 mother liquor Substances 0.000 description 1
- 229930027945 nicotinamide-adenine dinucleotide Natural products 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
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- 238000003305 oral gavage Methods 0.000 description 1
- 229910052763 palladium Inorganic materials 0.000 description 1
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- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
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- HDOWRFHMPULYOA-UHFFFAOYSA-N piperidin-4-ol Chemical compound OC1CCNCC1 HDOWRFHMPULYOA-UHFFFAOYSA-N 0.000 description 1
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- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- RSIJVJUOQBWMIM-UHFFFAOYSA-L sodium sulfate decahydrate Chemical compound O.O.O.O.O.O.O.O.O.O.[Na+].[Na+].[O-]S([O-])(=O)=O RSIJVJUOQBWMIM-UHFFFAOYSA-L 0.000 description 1
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- UOUFRTFWWBCVPV-UHFFFAOYSA-N tert-butyl 4-(2,4-dioxo-1H-thieno[3,2-d]pyrimidin-3-yl)piperidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCC(CC1)n1c(=O)[nH]c2ccsc2c1=O UOUFRTFWWBCVPV-UHFFFAOYSA-N 0.000 description 1
- HECDBBNAPNCHLX-UHFFFAOYSA-N tert-butyl 4-(3-fluoro-4-methoxyphenyl)-3,6-dihydro-2h-pyridine-1-carboxylate Chemical compound C1=C(F)C(OC)=CC=C1C1=CCN(C(=O)OC(C)(C)C)CC1 HECDBBNAPNCHLX-UHFFFAOYSA-N 0.000 description 1
- WUBVEMGCQRSBBT-UHFFFAOYSA-N tert-butyl 4-(trifluoromethylsulfonyloxy)-3,6-dihydro-2h-pyridine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCC(OS(=O)(=O)C(F)(F)F)=CC1 WUBVEMGCQRSBBT-UHFFFAOYSA-N 0.000 description 1
- JYUQEWCJWDGCRX-UHFFFAOYSA-N tert-butyl 4-formylpiperidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCC(C=O)CC1 JYUQEWCJWDGCRX-UHFFFAOYSA-N 0.000 description 1
- ROUYFJUVMYHXFJ-UHFFFAOYSA-N tert-butyl 4-oxopiperidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCC(=O)CC1 ROUYFJUVMYHXFJ-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (3)
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| US24544509P | 2009-09-24 | 2009-09-24 | |
| PCT/US2010/041645 WO2011008663A1 (en) | 2009-07-15 | 2010-07-12 | Gpr119 agonists |
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| SG177646A1 true SG177646A1 (en) | 2012-02-28 |
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| SG2012002523A SG177646A1 (en) | 2009-07-15 | 2010-07-12 | Gpr119 agonists |
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| Country | Link |
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| US (1) | US8207344B2 (enExample) |
| EP (1) | EP2454251A1 (enExample) |
| JP (1) | JP5715127B2 (enExample) |
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| CN (1) | CN102471313B (enExample) |
| AR (1) | AR077638A1 (enExample) |
| AU (1) | AU2010273642B2 (enExample) |
| BR (1) | BRPI1015921A2 (enExample) |
| CA (1) | CA2764906C (enExample) |
| CO (1) | CO6480977A2 (enExample) |
| CR (1) | CR20120012A (enExample) |
| DO (1) | DOP2012000006A (enExample) |
| EA (1) | EA020540B1 (enExample) |
| EC (1) | ECSP12011606A (enExample) |
| IL (1) | IL216776A0 (enExample) |
| MA (1) | MA33428B1 (enExample) |
| MX (1) | MX2012000704A (enExample) |
| NZ (1) | NZ597125A (enExample) |
| PE (1) | PE20121045A1 (enExample) |
| SG (1) | SG177646A1 (enExample) |
| TN (1) | TN2012000002A1 (enExample) |
| TW (1) | TWI429634B (enExample) |
| WO (1) | WO2011008663A1 (enExample) |
| ZA (1) | ZA201200227B (enExample) |
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| KR101078098B1 (ko) | 2003-01-14 | 2011-10-28 | 아레나 파마슈티칼스, 인크. | 대사 조절제로서의 １,２,３-삼치환된 아릴 및 헤테로아릴유도체, 및 당뇨병 및 고혈당증을 비롯한 이에 관련된장애의 예방 및 치료 |
| EP2108960A1 (en) | 2008-04-07 | 2009-10-14 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY |
| WO2011113947A1 (en) | 2010-03-18 | 2011-09-22 | Boehringer Ingelheim International Gmbh | Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions |
| SG188548A1 (en) | 2010-09-22 | 2013-04-30 | Arena Pharm Inc | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2012135570A1 (en) * | 2011-04-01 | 2012-10-04 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2012138845A1 (en) | 2011-04-08 | 2012-10-11 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment |
| WO2012170702A1 (en) * | 2011-06-08 | 2012-12-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2012170867A1 (en) | 2011-06-09 | 2012-12-13 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of gpr-119 |
| EP2720544B1 (en) | 2011-06-16 | 2016-12-21 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment |
| EP2760855B1 (en) * | 2011-09-30 | 2017-03-15 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds as well as their use in treating type-2 diabetes |
| WO2013062838A1 (en) | 2011-10-24 | 2013-05-02 | Merck Sharp & Dohme Corp. | Substituted piperidinyl compounds useful as gpr119 agonists |
| WO2013062835A1 (en) * | 2011-10-24 | 2013-05-02 | Merck Sharp & Dohme Corp. | Substituted piperidinyl compounds useful as gpr119 agonists |
| AU2012339870B2 (en) | 2011-11-15 | 2017-06-29 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds useful as GPR119 agonists |
| WO2013187646A1 (en) * | 2012-06-12 | 2013-12-19 | Chong Kun Dang Pharmaceutical Corp. | Piperidine derivatives for gpr119 agonist |
| CA2878625A1 (en) | 2012-07-11 | 2014-01-16 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| WO2014052619A1 (en) * | 2012-09-27 | 2014-04-03 | Irm Llc | Piperidine derivatives and compositions as modulators of gpr119 activity |
| CN110028494A (zh) * | 2013-11-26 | 2019-07-19 | 株式会社钟根堂 | 酰胺衍生物、其立体异构体或其药学上可接受的盐及包含其的药物组合物 |
| KR101651505B1 (ko) * | 2014-05-02 | 2016-08-29 | 현대약품 주식회사 | 싸이클로 헥센 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 대사성 질환의 예방 또는 치료용 약학적 조성물 |
| PL3242666T3 (pl) | 2015-01-06 | 2025-02-17 | Arena Pharmaceuticals, Inc. | Związek do zastosowania w leczeniu dolegliwości związanych z receptorem s1p1 |
| HUE060476T2 (hu) | 2015-06-22 | 2023-03-28 | Arena Pharm Inc | (R)-2-(7-(4-ciklopentil-3-(trifluormetil)benziloxi)-1,2,3,4- tetrahidrociklopenta[B]indol-3-il)ecetsav kristályos L-arginin-sója S1P1 receptorral kapcsolatos rendellenességek esetén való alkalmazásra |
| WO2018151873A1 (en) | 2017-02-16 | 2018-08-23 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of primary biliary cholangitis |
| US12156866B2 (en) | 2018-06-06 | 2024-12-03 | Arena Pharmaceuticals, Inc. | Methods of treating conditions related to the S1P1 receptor |
| PH12022552277A1 (en) | 2020-02-28 | 2024-03-04 | Kallyope Inc | Gpr40 agonists |
| JP2023526625A (ja) | 2020-05-19 | 2023-06-22 | キャリーオペ，インク． | Ａｍｐｋアクチベーター |
| CN116390925A (zh) | 2020-06-26 | 2023-07-04 | 卡尔优普公司 | Ampk活化剂 |
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| KR101078098B1 (ko) * | 2003-01-14 | 2011-10-28 | 아레나 파마슈티칼스, 인크. | 대사 조절제로서의 １,２,３-삼치환된 아릴 및 헤테로아릴유도체, 및 당뇨병 및 고혈당증을 비롯한 이에 관련된장애의 예방 및 치료 |
| CA2661371A1 (en) * | 2006-08-30 | 2008-03-06 | Biovitrum Ab (Publ) | Pyrimidine compounds for treating gpr119 related disorders |
| US7638541B2 (en) * | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| AU2008302570B2 (en) * | 2007-09-20 | 2012-05-31 | Irm Llc | Compounds and compositions as modulators of GPR119 activity |
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- 2010-07-12 MA MA34531A patent/MA33428B1/fr unknown
- 2010-07-12 MX MX2012000704A patent/MX2012000704A/es active IP Right Grant
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| NZ597125A (en) | 2013-08-30 |
| AR077638A1 (es) | 2011-09-14 |
| ZA201200227B (en) | 2013-06-26 |
| US8207344B2 (en) | 2012-06-26 |
| EP2454251A1 (en) | 2012-05-23 |
| TW201114757A (en) | 2011-05-01 |
| AU2010273642B2 (en) | 2014-03-13 |
| DOP2012000006A (es) | 2012-01-31 |
| US20110015199A1 (en) | 2011-01-20 |
| TN2012000002A1 (en) | 2013-09-19 |
| KR101365854B1 (ko) | 2014-02-21 |
| MX2012000704A (es) | 2012-03-07 |
| TWI429634B (zh) | 2014-03-11 |
| JP5715127B2 (ja) | 2015-05-07 |
| CA2764906C (en) | 2014-06-10 |
| MA33428B1 (fr) | 2012-07-03 |
| EA020540B1 (ru) | 2014-11-28 |
| BRPI1015921A2 (pt) | 2016-04-26 |
| CN102471313A (zh) | 2012-05-23 |
| CA2764906A1 (en) | 2011-01-20 |
| WO2011008663A1 (en) | 2011-01-20 |
| AU2010273642A1 (en) | 2012-01-19 |
| CO6480977A2 (es) | 2012-07-16 |
| CR20120012A (es) | 2012-03-28 |
| IL216776A0 (en) | 2012-03-01 |
| EA201270169A1 (ru) | 2012-06-29 |
| ECSP12011606A (es) | 2012-02-29 |
| CN102471313B (zh) | 2014-06-04 |
| PE20121045A1 (es) | 2012-08-09 |
| KR20120024964A (ko) | 2012-03-14 |
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